AU758968B2 - Non-peptide antagonists of GLP-1 receptor and methods of use - Google Patents
Non-peptide antagonists of GLP-1 receptor and methods of use Download PDFInfo
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- AU758968B2 AU758968B2 AU17518/00A AU1751800A AU758968B2 AU 758968 B2 AU758968 B2 AU 758968B2 AU 17518/00 A AU17518/00 A AU 17518/00A AU 1751800 A AU1751800 A AU 1751800A AU 758968 B2 AU758968 B2 AU 758968B2
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- 238000000034 method Methods 0.000 title claims abstract description 75
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 title claims abstract description 27
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 title claims abstract description 27
- 239000005557 antagonist Substances 0.000 title abstract description 21
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- 230000004913 activation Effects 0.000 claims abstract description 13
- 230000002401 inhibitory effect Effects 0.000 claims abstract description 10
- 108090000765 processed proteins & peptides Proteins 0.000 claims abstract description 8
- 239000002464 receptor antagonist Substances 0.000 claims abstract description 7
- 229940044551 receptor antagonist Drugs 0.000 claims abstract description 7
- 229910052739 hydrogen Inorganic materials 0.000 claims description 71
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- 239000001257 hydrogen Substances 0.000 claims description 70
- 125000001424 substituent group Chemical group 0.000 claims description 60
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- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims description 52
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- 101710176384 Peptide 1 Proteins 0.000 abstract 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11173698P | 1998-12-10 | 1998-12-10 | |
| US60/111736 | 1998-12-10 | ||
| PCT/US1999/029065 WO2000033839A1 (fr) | 1998-12-10 | 1999-12-08 | Antagonistes non peptidiques du recepteur glp-1 et techniques d'utilisation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU1751800A AU1751800A (en) | 2000-06-26 |
| AU758968B2 true AU758968B2 (en) | 2003-04-03 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU17518/00A Ceased AU758968B2 (en) | 1998-12-10 | 1999-12-08 | Non-peptide antagonists of GLP-1 receptor and methods of use |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US6469021B1 (fr) |
| EP (1) | EP1137413B1 (fr) |
| JP (1) | JP2002531501A (fr) |
| KR (1) | KR20010089563A (fr) |
| AT (1) | ATE288268T1 (fr) |
| AU (1) | AU758968B2 (fr) |
| BR (1) | BR9916965A (fr) |
| CA (1) | CA2350887A1 (fr) |
| DE (1) | DE69923587T2 (fr) |
| ES (1) | ES2233089T3 (fr) |
| NZ (1) | NZ511698A (fr) |
| PT (1) | PT1137413E (fr) |
| WO (1) | WO2000033839A1 (fr) |
| ZA (1) | ZA200104128B (fr) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001085256A2 (fr) | 2000-05-05 | 2001-11-15 | Novo Nordisk A/S | Maladie neurophatique grave |
| WO2002045712A1 (fr) * | 2000-12-04 | 2002-06-13 | Biovitrum Ab | Nouveau procede et nouvelle utilisation |
| AU2003203146A1 (en) * | 2002-02-07 | 2003-09-02 | Novo Nordisk A/S | Use of glp-1 compound for treatment of critically ill patients |
| US20030199445A1 (en) | 2002-02-07 | 2003-10-23 | Knudsen Lotte Bjerre | Use of GLP-1 compound for treatment of critically ill patients |
| DE60302336T2 (de) * | 2002-02-13 | 2006-08-03 | F. Hoffmann-La Roche Ag | Neue pyridin- und quinolin-derivate |
| CN100503607C (zh) * | 2003-06-02 | 2009-06-24 | 新疆华世丹药物研究有限责任公司 | 去氢骆驼蓬碱衍生物类化合物及其应用 |
| EP3456340B1 (fr) | 2007-01-08 | 2022-02-16 | The Trustees of the University of Pennsylvania | Antagonistes du récepteur du glp-1 pour l'utilisation dans le traitement de l'hyperinsulinisme familial |
| CA2700160A1 (fr) * | 2007-09-20 | 2009-03-26 | D2E, Llc | Derives a base de fluor de pyrido[4,3-b]indoles hydrogenes dotes de proprietes neuroprotectrices et favorisant la cognition, procede de preparation et utilisation |
| WO2009067233A1 (fr) * | 2007-11-20 | 2009-05-28 | Millennium Pharmaceuticals, Inc. | Bêta-carbolines et leurs utilisations |
| CA3024353A1 (fr) | 2015-05-22 | 2016-12-01 | The Bot Of The Leland Stanford Junior University | Traitement de l'hypoglycemie post-bariatrique avec des antagonistes glp-1 |
| WO2017152014A1 (fr) | 2016-03-04 | 2017-09-08 | Eiger Biopharmaceuticals, Inc. | Traitement de l'hypoglycémie hyperinsulinémique avec des dérivés de l'exendine-4 |
| EP3541366A4 (fr) | 2016-11-21 | 2020-08-05 | Eiger Biopharmaceuticals, Inc. | Formulations tamponnées d'exendine (9-39) |
| CN111362937B (zh) * | 2020-03-06 | 2021-06-22 | 贵州医科大学 | N-芳基-β-卡波林类衍生物及其用途 |
| KR20230043885A (ko) * | 2020-07-23 | 2023-03-31 | 메르크 파텐트 게엠베하 | 트리시클릭 헤테로사이클 |
| US20230390250A1 (en) * | 2020-10-30 | 2023-12-07 | Robin Elaine DUNCAN | Modulation of glucagon-like peptide 1 and uses thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5834482A (en) * | 1995-05-05 | 1998-11-10 | Novo Nordisk A/S | Heterocyclic chemistry |
-
1999
- 1999-12-08 BR BR9916965-7A patent/BR9916965A/pt not_active IP Right Cessation
- 1999-12-08 ES ES99960663T patent/ES2233089T3/es not_active Expired - Lifetime
- 1999-12-08 PT PT99960663T patent/PT1137413E/pt unknown
- 1999-12-08 EP EP99960663A patent/EP1137413B1/fr not_active Expired - Lifetime
- 1999-12-08 US US09/831,572 patent/US6469021B1/en not_active Expired - Fee Related
- 1999-12-08 JP JP2000586331A patent/JP2002531501A/ja active Pending
- 1999-12-08 AU AU17518/00A patent/AU758968B2/en not_active Ceased
- 1999-12-08 WO PCT/US1999/029065 patent/WO2000033839A1/fr active IP Right Grant
- 1999-12-08 DE DE69923587T patent/DE69923587T2/de not_active Expired - Fee Related
- 1999-12-08 NZ NZ511698A patent/NZ511698A/en unknown
- 1999-12-08 AT AT99960663T patent/ATE288268T1/de not_active IP Right Cessation
- 1999-12-08 CA CA002350887A patent/CA2350887A1/fr not_active Abandoned
- 1999-12-08 KR KR1020017007173A patent/KR20010089563A/ko not_active Application Discontinuation
-
2001
- 2001-05-21 ZA ZA200104128A patent/ZA200104128B/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5834482A (en) * | 1995-05-05 | 1998-11-10 | Novo Nordisk A/S | Heterocyclic chemistry |
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| Title |
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| KELLY T.R. ET AL., TETRAHEDRON LETTERS 34(1993) PP 6173-6176 * |
| VOELKER T ET AL., TETRAHEDRON LETTERS 39(1998) PP 359-362 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1137413B1 (fr) | 2005-02-02 |
| EP1137413A2 (fr) | 2001-10-04 |
| ATE288268T1 (de) | 2005-02-15 |
| ZA200104128B (en) | 2002-05-21 |
| EP1137413A4 (fr) | 2002-06-26 |
| KR20010089563A (ko) | 2001-10-06 |
| WO2000033839B1 (fr) | 2000-09-28 |
| DE69923587D1 (de) | 2005-03-10 |
| BR9916965A (pt) | 2001-11-06 |
| JP2002531501A (ja) | 2002-09-24 |
| AU1751800A (en) | 2000-06-26 |
| DE69923587T2 (de) | 2005-06-23 |
| NZ511698A (en) | 2003-09-26 |
| ES2233089T3 (es) | 2005-06-01 |
| WO2000033839A1 (fr) | 2000-06-15 |
| PT1137413E (pt) | 2005-05-31 |
| CA2350887A1 (fr) | 2000-06-15 |
| US6469021B1 (en) | 2002-10-22 |
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